XAV-939 - ≥98%, high purity , CAS No.284028-89-3

  • ≥98%
Item Number
X125899
Grouped product items
SKUSizeAvailabilityPrice Qty
X125899-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$58.90
X125899-10mg
10mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$70.90
X125899-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$159.90
X125899-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$331.90
X125899-250mg
250mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$747.90

Potent tankyrase inhibitor. Inhibitor of Wnt/β-catenin signaling.

Basic Description

Synonyms2-(4-(Trifluoromethyl)phenyl)-3,5,7,8-tetrahydro-4H-thiopyrano[4,3-d]pyrimidin-4-one | EN300-6732792 | BCPP000009 | SW218311-2 | SB19432 | 2-[4-(Trifluoromethyl)phenyl]-7,8-Dihydro-5h-Thiopyrano[4,3-D]pyrimidin-4-Ol | AC-28393 | BCP02128 | CHEBI:62878 | H
Specifications & Purity≥98%
Biochemical and Physiological MechanismsXAV939 is a potent, small molecule inhibitor of tankyrase 1 (TNKS) (IC50 = 11 nM) and tankyrase 2 (IC50 = 4 nM). By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
A potent inhibitor of beta-catenin, TNKS1, and TNKS2.

Associated Targets(Human)

TNKS Tchem Tankyrase-1 (20 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PARP3 Tclin Poly [ADP-ribose] polymerase 3 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PARP1 Tclin Poly [ADP-ribose] polymerase 1 (8 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PARP2 Tclin Poly [ADP-ribose] polymerase 2 (9 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
AXIN2 Tchem Axin-2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
WNT3A Tchem Protein Wnt-3a (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TNKS2 Tchem Tankyrase-2 (21 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
IMPDH2 Tclin Inosine-5'-monophosphate dehydrogenase 2 (1326 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PARP1 Tclin Poly [ADP-ribose] polymerase-1 (6206 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
COLO 320DM (191 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SW480 (6023 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
A549 (127892 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PARP2 Tclin Poly [ADP-ribose] polymerase 2 (1185 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PARP3 Tclin Poly [ADP-ribose] polymerase 3 (206 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TNKS Tchem Tankyrase-1 (1241 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsomes (16955 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PARP4 Tchem Poly [ADP-ribose] polymerase 4 (71 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TNKS2 Tchem Tankyrase-2 (1531 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AXIN1 Tbio Axin-1 (7 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PARP14 Tchem Poly [ADP-ribose] polymerase 14 (380 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PARP15 Tchem Poly [ADP-ribose] polymerase 15 (178 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PARP6 Tchem Poly [ADP-ribose] polymerase 6 (23 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PARP11 Tbio Poly [ADP-ribose] polymerase 11 (83 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PARP10 Tchem Poly [ADP-ribose] polymerase 10 (418 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TNKS2 Tchem Tankyrase 1/2 (384 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PARP16 Tchem Mono [ADP-ribose] polymerase PARP16 (46 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Wnt3a Protein Wnt-3a (429 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Axin2 Axin-2 (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Tnks Tankyrase (8 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 2-[4-(trifluoromethyl)phenyl]-3,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidin-4-one
INCHI InChI=1S/C14H11F3N2OS/c15-14(16,17)9-3-1-8(2-4-9)12-18-11-5-6-21-7-10(11)13(20)19-12/h1-4H,5-7H2,(H,18,19,20)
InChi Key KLGQSVMIPOVQAX-UHFFFAOYSA-N
Canonical SMILES C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F
Isomeric SMILES C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F
WGK Germany 3
PubChem CID 135418940
Molecular Weight 312.31

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

5 results found

Lot NumberCertificate TypeDateItem
L1828016Certificate of AnalysisJun 19, 2024 X125899
L2301172Certificate of AnalysisDec 07, 2023 X125899
L2301171Certificate of AnalysisDec 07, 2023 X125899
A2206323Certificate of AnalysisOct 24, 2023 X125899
L1828017Certificate of AnalysisOct 18, 2022 X125899

Chemical and Physical Properties

SolubilitySoluble in 1:5 EtOH:PBS (pH 7.2) (~0.15 mg/ml), DMSO (~2 mg/ml), DMF (~5 mg/ml), water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25 °C.
SensitivityHeat Sensitive

Safety and Hazards(GHS)

Pictogram(s) GHS06,   GHS07
Signal Danger
Hazard Statements

H319:Causes serious eye irritation

H301:Toxic if swallowed

Precautionary Statements

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P321:Specific treatment (see ... on this label).

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P270:Do not eat, drink or smoke when using this product.

P330:Rinse mouth.

P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes.

P301+P316:IF SWALLOWED: Get emergency medical help immediately.

P337+P317:If eye irritation persists: Get medical help.

WGK Germany 3

Related Documents

Citations of This Product

1. Xin Wang, Shoulin Li, Cheng Zhang, Wenping Xu, Mengqi Wu, Jiagao Cheng, Zhong Li, Liming Tao, Yang Zhang.  (2024)  Stereoselective toxicity of acetochlor chiral isomers on the nervous system of zebrafish larvae.  JOURNAL OF HAZARDOUS MATERIALS,  464  (15): (133016).  [PMID:37992503] [10.1016/j.jhazmat.2023.133016]
2. Yuan Xu, Jian He, Jun He.  (2022)  Cyanidin attenuates the high hydrostatic pressure-induced degradation of cellular matrix of nucleus pulposus cell via blocking the Wnt/β-catenin signaling.  TISSUE & CELL,  76  (101798).  [PMID:35472676] [10.1016/j.tice.2022.101798]
3. Chen Gang, Chen Weicheng, Ye Ming, Tan Weiqiang, Jia Bing.  (2019)  TRIM59 knockdown inhibits cell proliferation by down-regulating the Wnt/β-catenin signaling pathway in neuroblastoma.  BIOSCIENCE REPORTS,  39  (1):   [PMID:30389710] [10.1042/BSR20181277]

References

1. Fagnocchi L et al..  (2016)  A Myc-driven self-reinforcing regulatory network maintains mouse embryonic stem cell identity..  Nat Commun,  (11903).  [PMID:27301576]
2. Polley A et al..  (2020)  Asporin Reduces Adult Aortic Valve Interstitial Cell Mineralization Induced by Osteogenic Media and Wnt Signaling Manipulation In Vitro..  Int J Cell Biol,  2020  (2045969).  [PMID:32328102]
3. Du B et al..  (2020)  Long non-coding RNA MALAT1 suppresses the proliferation and migration of endothelial progenitor cells in deep vein thrombosis by regulating the Wnt/ß-catenin pathway..  Exp Ther Med,  20  (4): (3138-3146).  [PMID:32855682]
4. Hamidi S et al..  (2020)  Mesenchymal-epithelial transition regulates initiation of pluripotency exit before gastrulation..  Development,  147  (3):   [PMID:32014865]
5. Lafon-Hughes L et al..  (2014)  VERO cells harbor a poly-ADP-ribose belt partnering their epithelial adhesion belt..  PeerJ,  (e617).  [PMID:25332845]
6. Xin Wang, Shoulin Li, Cheng Zhang, Wenping Xu, Mengqi Wu, Jiagao Cheng, Zhong Li, Liming Tao, Yang Zhang.  (2024)  Stereoselective toxicity of acetochlor chiral isomers on the nervous system of zebrafish larvae.  JOURNAL OF HAZARDOUS MATERIALS,  464  (15): (133016).  [PMID:37992503] [10.1016/j.jhazmat.2023.133016]
7. Yuan Xu, Jian He, Jun He.  (2022)  Cyanidin attenuates the high hydrostatic pressure-induced degradation of cellular matrix of nucleus pulposus cell via blocking the Wnt/β-catenin signaling.  TISSUE & CELL,  76  (101798).  [PMID:35472676] [10.1016/j.tice.2022.101798]
8. Chen Gang, Chen Weicheng, Ye Ming, Tan Weiqiang, Jia Bing.  (2019)  TRIM59 knockdown inhibits cell proliferation by down-regulating the Wnt/β-catenin signaling pathway in neuroblastoma.  BIOSCIENCE REPORTS,  39  (1):   [PMID:30389710] [10.1042/BSR20181277]

Solution Calculators